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Assay Detail

CHEMBL1780896

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Binding
Inhibition of MK2 in human THP1 cells assessed as Hsp27 phosphorylation
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type THP-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

MAP kinase-activated protein kinase 2 (CHEMBL2208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based lead identification of ATP-competitive MK2 inhibitors.
Barf T, Kaptein A, de Wilde S, van der Heijden R, van Someren R, Demont D, Schultz-Fademrecht C, Versteegh J, van Zeeland M, Seegers N, Kazemier B, van de Kar B, van Hoek M, de Roos J, Klop H, Smeets R, Hofstra C, Hornberg J, Oubrie A.
Bioorg Med Chem Lett (2011) 21 : 3818 -3822
PubMed 21565500 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 6.21 6.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1738702 1 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1738702 EC50 = 620.0 nM 6.21